姜黄素-PLGA纳米粒提高口服给药生物利用度的研究

Enhancement of Oral Bioavailability of Curcumin Loaded PLGA Nanoparticles

关键词:  姜黄素  姜黄素纳米粒  生物利用度  口服给药

Key words:  curcumin  curcumin nanoparticles  bioavailability  oral administration

摘要:

目的 研究乳酸/羟基乙酸共聚物(PLGA)纳米粒子提高姜黄素口服生物利用度。方法 采用乳液挥发法制备姜黄素-PLGA纳米粒；通过透射电镜(transmission electron microscope，TEM)观察纳米粒形态；采用动态光散射法(dynamic light scattering，DLS)测定纳米粒大小、表面电位(Zeta电位)；考察药物的体外稳定性以及药物释放行为；以大鼠口服灌胃给药方式考察姜黄素和姜黄素-PLGA纳米粒的体内药物生物利用度。结果 姜黄素-PLGA纳米粒粒度分布均匀，平均粒径大小约200 nm；姜黄素-PLGA纳米粒具有较高的载药量和包封率以及稳定性，体外药物释放实验结果显示具有一定的缓释效果；口服灌胃100 mg·kg^-1姜黄素和姜黄素-PLGA纳米粒，给药30 min之后，姜黄素-PLGA纳米粒给药组的血药浓度水平显著高于姜黄素组(P<0.05)，药物生物利用度提高到原来的5.2倍。结论 姜黄素-PLGA纳米粒可以有效的提高姜黄素稳定性和口服给药生物利用度。

Abstract:

OBJECTIVE To investigate the enhancement of oral bioavailability of curcumin loaded PLGA nanoparticles. METHODS Curcumin loaded PLGA nanoparticle was developed by a emulsion method, and then characterized by a DLS, TEM and zeta potential. In vitro release study and in vitro stability test were also examined. The oral bioavailability study of curcumin and curcumin loaded PLGA nanoparticles was performed after the oral administration. RESULTS Curcumin loaded PLGA nanoparticles had mean diameter of 200 nm with uniform size distribution. And the developed nanoparticles with improvement of stability of curcumin had high drug encapsulation efficiency and drug loading capacity. In vitro release study showed that curcumin was sustained release from nanoparticles. After 30 min of oral administration of curcumin or curcumin loaded PLGA nanoparticles (100 mg·kg^-1), the blood concentration of curcumin loaded PLGA nanoparticles group showed great significance with that of curcumin group. The bioavailability of curcumin was enhanced 5.2-fold in curcumin loaded PLGA nanoparticles groups as compared with curcumin group. CONCLUSION Curcumin loaded PLGA nanoparticles could greatly improve the stability of curcumin and oral bioavailability of curcumin.